CA2506290C - 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases - Google Patents

17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases Download PDF

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Publication number
CA2506290C
CA2506290C CA2506290A CA2506290A CA2506290C CA 2506290 C CA2506290 C CA 2506290C CA 2506290 A CA2506290 A CA 2506290A CA 2506290 A CA2506290 A CA 2506290A CA 2506290 C CA2506290 C CA 2506290C
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CA
Canada
Prior art keywords
compound
isomer
pharmaceutically acceptable
solvate
acceptable salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA2506290A
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English (en)
French (fr)
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CA2506290A1 (en
Inventor
Kamil Paruch
Timothy J. Guzi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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Publication of CA2506290A1 publication Critical patent/CA2506290A1/en
Application granted granted Critical
Publication of CA2506290C publication Critical patent/CA2506290C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/12Keratolytics, e.g. wart or anti-corn preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Steroid Compounds (AREA)
CA2506290A 2002-11-18 2003-11-14 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases Expired - Fee Related CA2506290C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42726302P 2002-11-18 2002-11-18
US60/427,263 2002-11-18
PCT/US2003/036203 WO2004046111A1 (en) 2002-11-18 2003-11-14 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases

Publications (2)

Publication Number Publication Date
CA2506290A1 CA2506290A1 (en) 2004-06-03
CA2506290C true CA2506290C (en) 2012-04-24

Family

ID=32326512

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2506290A Expired - Fee Related CA2506290C (en) 2002-11-18 2003-11-14 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases

Country Status (16)

Country Link
US (2) US7074795B2 (https=)
EP (1) EP1562901B1 (https=)
JP (2) JP4614770B2 (https=)
CN (1) CN100374421C (https=)
AR (1) AR042046A1 (https=)
AT (1) ATE469886T1 (https=)
AU (1) AU2003290799A1 (https=)
CA (1) CA2506290C (https=)
CL (1) CL2003002356A1 (https=)
DE (1) DE60332862D1 (https=)
ES (1) ES2345146T3 (https=)
MX (1) MXPA05005360A (https=)
MY (1) MY130792A (https=)
PE (1) PE20040750A1 (https=)
TW (1) TW200412964A (https=)
WO (1) WO2004046111A1 (https=)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA05006485A (es) 2002-12-17 2005-08-26 Schering Corp Inhibidores de la 17 beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgeno.
GB0513702D0 (en) 2005-07-04 2005-08-10 Sterix Ltd Compound
US7851474B2 (en) * 2005-08-02 2010-12-14 Neurogen Corporation Dipiperazinyl ketones and related analogues
US8080540B2 (en) 2006-09-19 2011-12-20 Abbott Products Gmbh Therapeutically active triazoles and their use
US8288367B2 (en) 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
US8501940B2 (en) * 2008-07-15 2013-08-06 Hoffmann-La Roche Inc. Tetrahydrocinnoline derivatives
CN103596550A (zh) * 2011-04-25 2014-02-19 朴俊炯 用于预防脱发和促进毛发生长的局部施用的组合物
WO2014207311A1 (en) 2013-06-25 2014-12-31 Forendo Pharma Ltd Therapeutically active estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxy-steroid dehydrogenase, type 1
US10377791B2 (en) 2013-06-25 2019-08-13 Forendo Pharma Ltd. Therapeutically active estratrienthiazole derivatives as inhibitors of 17 B-hydroxysteroid dehydrogenase, type 1
KR20160042873A (ko) 2013-06-25 2016-04-20 포렌도 파마 리미티드 17.베타.-하이드록시스테로이드 탈수소효소의 억제제로서 치료적 활성 17-질소 치환된 에스트라트리엔티아졸 유도체
CN107207561B (zh) 2014-12-23 2020-03-31 佛恩多制药有限公司 17β-HSD1–抑制剂的前药
US10626140B2 (en) 2014-12-23 2020-04-21 Forendo Pharma Ltd Prodrugs of 17β-HSD1-inhibitors
HK1249504A1 (zh) 2015-09-02 2018-11-02 Glaxosmithkline Intellectual Property (No. 2) Limited 用作溴结构域抑制剂的吡啶酮二甲酰胺
FI3634975T3 (fi) 2017-06-08 2024-05-03 Organon R&D Finland Ltd 15-beeta-[3-propanamido]substituoitujen estra-1,3,5(10)-trien-17-onien 17-oksiimeja käytettäväksi 17-beeta-hydroksisteroididehydrogenaasien inhiboimisessa
EP3724178B1 (en) * 2017-12-15 2024-05-01 Inthera Bioscience AG 1-(piperidinocarbonylmethyl)-2-oxopiperazine derivatives for treating cancer
BR112021010598A2 (pt) 2018-12-05 2021-08-24 Forendo Pharma Ltd Compostos, método para preparação de um composto e composição farmacêutica

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3586053D1 (de) 1984-08-02 1992-06-17 Labrie Pharmazeutische zusammensetzung fuer die kombinationstherapie von hormonabhaengigem krebs.
ES2077675T3 (es) 1989-03-10 1995-12-01 Endorecherche Inc Terapia combinada para el tratamiento de enfermedades sensibles a los estrogenos.
ATE269066T1 (de) 1989-07-07 2004-07-15 Endorech Inc Kombinationstherapie zur prophylaxe und/oder behandlung von gutartiger prostatischer hyperplasie
HUT60139A (en) 1989-07-07 1992-08-28 Endorecherche Inc Process for producing pharmaceutical composition suitable for treating prostate cancer connected with androgen
US6060503A (en) 1991-12-02 2000-05-09 Endorecherche, Inc. Benzopyran-containing compounds and method for their use
SK139194A3 (en) 1993-05-17 1995-07-11 Endorecherche Inc The improved antiandrogens
US6124115A (en) 1995-09-22 2000-09-26 Endorecherche Inc. Production and use of isolated type 5 17β-hydroxysteroid dehydrogenase
AU4801197A (en) * 1996-09-13 1998-04-02 Schering Corporation Tricyclic antitumor compounds being farnesyl protein transferase inhibit ors
TR200002784T2 (tr) 1998-03-11 2000-12-21 Endorecherche, Inc Tip 5 ve tip 3 17beta-Hidroksisteroid dehidrojenaz inhibitörleri ve bunların kullanımı için metodlar
AR036492A1 (es) * 2001-09-06 2004-09-15 Schering Corp Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos inhibidores para la elaboracion de un medicamento para el tratamiento de enfermedades androgeno dependientes
MXPA04003611A (es) 2001-10-17 2004-07-30 Schering Corp Piperidina- y piperazinacetaminas como inhibidores de la 17 beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades androgeno-dependientes.

Also Published As

Publication number Publication date
CA2506290A1 (en) 2004-06-03
CN100374421C (zh) 2008-03-12
CN1738800A (zh) 2006-02-22
EP1562901A1 (en) 2005-08-17
JP2010138204A (ja) 2010-06-24
MY130792A (en) 2007-07-31
ES2345146T3 (es) 2010-09-16
PE20040750A1 (es) 2004-11-06
TW200412964A (en) 2004-08-01
AR042046A1 (es) 2005-06-08
US7074795B2 (en) 2006-07-11
HK1073313A1 (en) 2005-09-30
AU2003290799A1 (en) 2004-06-15
US20060148816A1 (en) 2006-07-06
US7476681B2 (en) 2009-01-13
CL2003002356A1 (es) 2005-02-11
JP4614770B2 (ja) 2011-01-19
ATE469886T1 (de) 2010-06-15
DE60332862D1 (de) 2010-07-15
JP2006513169A (ja) 2006-04-20
EP1562901B1 (en) 2010-06-02
US20040127503A1 (en) 2004-07-01
MXPA05005360A (es) 2005-08-03
WO2004046111A1 (en) 2004-06-03

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EEER Examination request
MKLA Lapsed

Effective date: 20141114